688001

Y-27632

≥95% (HPLC), liquid, Rho kinase inhibitor, Calbiochem^®

• 동의어(들): InSolution Y-27632, Rho Kinase Inhibitor VI
• 실험식(Hill 표기법): C₁₄H₂₁N₃O · 2HCl · xH₂O
• Molecular Weight: 320.26 (anhydrous basis)
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• product name: Y-27632, InSolution, ≥95%, reversible, inhibitor of Rho kinases
• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: liquid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 배송 상태: wet ice
• 저장 온도: −20°C

설명

일반 설명

A 5 mM (500 µg/296 µl) aqueous solution of Y-27632 (Cat. No. 688000). A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (K_i = 140 nM for p160^ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKC_ε than p160^ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 mM). Also acts as a potent inhibitor of agonist-induced Ca²⁺ sensitization of myosin phosphorylation and smooth muscle contractions (IC₅₀ = 700 nM for phenylephrine-induced contractions in aortic strips).

A highly potent, cell-permeable, selective inhibitor of Rho-associated protein kinase (K_i = 140 nM for p160^ROCK (ROCK-I). Also inhibits ROCK-II with almost equal potency. Inhibition is achieved by competing with ATP for binding to the catalytic site. Exhibits 10- to 50-fold lower affinity for PKC_ε than p160^ROCK. Does not affect the activity of p21-activated protein kinase (PAK) even at high concentrations (~100 mM). Also acts as a potent inhibitor of agonist-induced Ca²⁺ sensitization of myosin phosphorylation and smooth muscle contractions (IC₅₀ = 700 nM for phenylephrine-induced contractions in aortic strips).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
p160ROCK

Product competes with ATP.

Reversible: no

Target IC₅₀: 700 nM against phenylephrine-induced contractions in aortic strips

Target K_i: 140 nM for p160ROCK (ROCK-I)

포장

Packaged under inert gas

경고

Toxicity: Harmful (C)

물리적 형태

A 5 mM (500 µg/296 µl) solution of Y-27632 (Cat. No. 688000) in H₂O.

재구성

Following initial thaw, aliquot and freeze (-20°C).

기타 정보

Chitaley, K., et al. 2001. Nat. Med.7, 119.
Davies, S.P., et al. 2000. Biochem. J. 351, 95.
Narumiya, S., et al. 2000. Methods Enzymol.325, 273.
Hirose, M., et al. 1999. J. Cell Biol.141, 1625.
Maekawa, M., et al. 1999. Science285, 895.
Uehata, M., et al. 1997. Nature389, 990.

법적 정보

Sold under license of PCT Application W098/06,433A1 and under license from Mitsubishi Pharma Tanabe Corporation.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 12 - Non Combustible Liquids
• WGK: WGK 2
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable